Heavy Metal, Aluminum, Boron Or Silicon Containing Patents (Class 540/452)
  • Patent number: 9441059
    Abstract: The present application provides, among other things, compounds and methods for metathesis reactions. In some embodiments, a provided compound has the structure of formula I, II or III. In some embodiments, R1 of formula I, II or III comprises an electron-withdrawing group. In some embodiments, the present invention provides methods for preparing provided compounds.
    Type: Grant
    Filed: June 20, 2014
    Date of Patent: September 13, 2016
    Assignee: Massachusetts Institute of Technology
    Inventors: Richard Royce Schrock, Jian Yuan, Jonathan Clayton Axtell
  • Patent number: 8754206
    Abstract: The present invention discloses metal (III) complex of a biuret-amide based macrocyclic ligand as green catalysts that exhibit both excellent reactivity for the activation of H2O2 and high stability at low pH and high ionic strength. The invention also provides macrocyclic biuret amide based ligand for designing of functional peroxidase mimics. Further, the present invention discloses synthesis of said metal (III) complex of a biuret-amide based macrocyclic ligand.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: June 17, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Sayam Sengupta, Chakadola Panda, Munmun Ghosh
  • Patent number: 8722881
    Abstract: A tetradendate amide based macrocyclic ligand and its Fe(III) complex which act as activators of hydrogen peroxide. The synthetic methodology to develop the ligands is new, simple and provides better yield for each step of the ligand synthesis. The Fe(III)-complexes and hydrogen peroxide together are can perform several environmentally benign oxidation reactions. Organic dye bleaching, bleaching of pulp and paper effluent and N-oxide synthesis may be performed using the newly developed catalyst and hydrogen peroxide. Alcohol oxidation and alkene epoxidation may also be performed using the catalysts and hydrogen peroxide.
    Type: Grant
    Filed: October 13, 2010
    Date of Patent: May 13, 2014
    Assignee: Board of Trustees of the University of Arkansas
    Inventors: Anindya Ghosh, Shane Z. Sullivan, Samuel L. Collom, Sharon Pulla
  • Publication number: 20140030221
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: June 7, 2013
    Publication date: January 30, 2014
    Inventors: Caroline Aciro, Victoria Alexandra Steadman, Simon Neil Pettit, Karine G. Poullennec, Linos Lazarides, David Kenneth Dean, Neil Andrew Dunbar, Adrian John Highton, Andrew John Keats, Dustin Scott Siegel, Kapil Kumar karki, Adam James Schrier, Petr Jansa, Richard Mackman
  • Publication number: 20120329680
    Abstract: The present invention discloses metal (III) complex of a biuret-amide based macrocyclic ligand as green catalysts that exhibit both excellent reactivity for the activation of H2O2 and high stability at low pH and high ionic strength. The invention also provides macrocyclic biuret amide based ligand for designing of functional peroxidase mimics. Further, the present invention discloses synthesis of said metal (III) complex of a biuret-amide based macrocyclic ligand.
    Type: Application
    Filed: May 23, 2012
    Publication date: December 27, 2012
    Inventors: Sayam Sengupta, Chakadola Panda, Munmun Ghosh
  • Publication number: 20120323000
    Abstract: The present invention relates generally to olefin metathesis. In some embodiments, the present invention provides methods for Z-selective ring-closing metathesis.
    Type: Application
    Filed: June 1, 2012
    Publication date: December 20, 2012
    Applicants: TRUSTEES OF BOSTON COLLEGE, MASSACHUSETTS INSTITUTE OF TECHNOLOGY
    Inventors: Amir H. Hoveyda, Miao Yu, Chenbo Wang, Richard R. Schrock
  • Publication number: 20120214253
    Abstract: The present invention provides a novel class of macrocyclic compounds as well as complexes formed between a metal (e.g., lanthanide) ion and the compounds of the invention. Preferred complexes exhibit high stability as well as high quantum yields of lanthanide ion luminescence in aqueous media without the need for secondary activating agents. Preferred compounds comprise hydroxypyridinonyl moieties within their macrocyclic structure and are characterized by surprisingly low, non-specific binding to a variety of polypeptides such as antibodies and proteins as well as high kinetic stability.
    Type: Application
    Filed: August 24, 2010
    Publication date: August 23, 2012
    Applicant: LUMIPHORE, INC.
    Inventors: Nathaniel G. Butlin, Kenneth N. Raymond, Jide Xu, Anthony D'Aleo
  • Publication number: 20110094043
    Abstract: A tetradendate amide based macrocyclic ligand and its Fe(III) complex which act as activators of hydrogen peroxide. The synthetic methodology to develop the ligands is new, simple and provides better yield for each step of the ligand synthesis. The Fe(III)-complexes and hydrogen peroxide together are can perform several environmentally benign oxidation reactions. Organic dye bleaching, bleaching of pulp and paper effluent and N-oxide synthesis may be performed using the newly developed catalyst and hydrogen peroxide. Alcohol oxidation and alkene epoxidation may also be performed using the catalysts and hydrogen peroxide.
    Type: Application
    Filed: October 13, 2010
    Publication date: April 28, 2011
    Inventors: Anindya Ghosh, Shane Z. Sullivan, Samuel L. Collom, Sharon Pulla
  • Publication number: 20100292464
    Abstract: A novel optical-isomer separating agent for chromatography is provided which has, as a chiral selector, a macrocyclic amide compound having the ability to function as a chiral shift agent. The optical-isomer separating agent for chromatography is formed by bonding, with a carrier by chemical bonding, a specific ring structure containing an asymmetry recognition site, an amide group as a hydrogen-bond donor site, and a hydrogen-bond acceptor site.
    Type: Application
    Filed: January 30, 2009
    Publication date: November 18, 2010
    Inventors: Tadashi Ema, Takashi Sakai, Daisuke Tanida, Kyoko Sugita, Atsushi Ohnishi, Kenichiro Miyazawa
  • Publication number: 20100167289
    Abstract: The present invention provides a novel class of macrocyclic compounds as well as complexes formed between a metal (e.g., lanthanide) ion and the compounds of the invention. Preferred complexes exhibit high stability as well as high quantum yields of lanthanide ion luminescence in aqueous media without the need for secondary activating agents. Preferred compounds incorporate hydroxy-isophthalamide moieties within their macrocyclic structure and are characterized by surprisingly low, non-specific binding to a variety of polypeptides such as antibodies and proteins as well as high kinetic stability. These characteristics distinguish them from known, open-structured ligands.
    Type: Application
    Filed: January 25, 2008
    Publication date: July 1, 2010
    Inventors: Nathaniel G. Butlin, Todd M. Corneillie, Jide Xu
  • Publication number: 20100120716
    Abstract: Macrocyclic inhibitors of Hepatitis C protease are provided, the inhibitors including a boronic acid or ester group, a macrocyclic ring of about 13 to 25 atoms including at least two amide linkages, a proline-analogous group, and a connecting segment joining moieties on either side of the proline-analogous group. Methods of making the HCV protease-inhibitory compounds, methods of using the compounds, formulations of the compounds, and pharmaceutical combinations including the compounds, are provided.
    Type: Application
    Filed: December 5, 2007
    Publication date: May 13, 2010
    Applicant: Phenomix Corporation
    Inventors: David A. Campbell, Michael E. Hepperle, David T. Winn, Juan M. Betancort
  • Publication number: 20090246763
    Abstract: Disclosed are tri-nuclear metal complexes and salts thereof, such as tri-nuclear osmium or ruthenium complexes or salts thereof, suitable for use as electrochemical labels. Also disclosed are oligonucleotide probes with an attached electrochemical label, methods of nucleic acid amplification, methods of sequencing, and kits for nucleic acid amplification and sequencing having oligonucleotide probes including an electrochemical label. The electrochemical labels are synthesized from siderophores.
    Type: Application
    Filed: March 31, 2008
    Publication date: October 1, 2009
    Applicant: APPLERA CORPORATION, APPLIED BIOSYSTEMS GROUP
    Inventor: Robert G. Eason
  • Publication number: 20080108694
    Abstract: The present invention relates to compounds having the structure (and pharmaceutically acceptable derivatives thereof) wherein Ro-R4, Z, X, A-B, D-E, G-J, and K-L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.
    Type: Application
    Filed: December 17, 2004
    Publication date: May 8, 2008
    Inventors: Samuel J Danishefsky, Zhi-Qiang Yang, Xudong Geng, Ting-Chao Chou, Neal Rosen
  • Patent number: 7241755
    Abstract: The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
    Type: Grant
    Filed: August 30, 2006
    Date of Patent: July 10, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson
  • Patent number: 7087384
    Abstract: The invention relates to a process for reducing the fluorescence quenching caused by the measuring medium in a fluorescence assay, by introducing into said medium of rare earth metal cryptates which are not very sensitive to this fluorescence quenching, said rare earth metal cryptates comprising at least one pyridine radical which is substituted one or more times or unsubstituted. The invention also relates to novel rare earth metal cryptates which are not very sensitive to the fluorescence quenching caused by the measuring medium.
    Type: Grant
    Filed: June 12, 2001
    Date of Patent: August 8, 2006
    Assignee: CIS bio international
    Inventors: Herve Autiero, Herve Bazin, Gerard Mathis
  • Patent number: 6962992
    Abstract: The invention describes crown ether chelators, including crown ethers having the formula and aza-substituted and thia-substituted analogs thereof. These crown ethers are substituted by a dye moiety, a chemically reactive group, a conjugated substance, or a combination thereof. Chelators that are substituted by fluorescent dyes are particularly useful as indicators for metal cations, particularly Na+ and K+ ions, and particularly where binding of the target ion results in a change in the fluorescence properties of the indicator that can be correlated with the ion concentration. Methods are provided for utilizing reactive groups on the chelators for conjugation to dyes, lipids and polymers and methods for enhancing entry of the indicators into living cells.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: November 8, 2005
    Assignee: Molecullar Probes, Inc.
    Inventors: Vladimir V. Martin, Kyle R. Gee, Richard P. Haugland, Zhenjun Diwu
  • Patent number: 6657057
    Abstract: The present invention provides an industrially excellent and novel process for producing methylcobalamin useful as medicines. Namely, it provides a process for producing methylcobalamin, which comprises the step of methylating cyanocobalamin or hydroxocobalamin in the presence of a reducing agent and a water-soluble methylating agent.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: December 2, 2003
    Assignee: Eisai Co., Ltd.
    Inventors: Yoshihiko Hisatake, Hiroshi Kuroda
  • Publication number: 20030212268
    Abstract: Provided are cucurbituril derivatives having the formula (1), their preparation methods and uses: 1
    Type: Application
    Filed: March 4, 2003
    Publication date: November 13, 2003
    Inventors: Kimoon Kim, Jianzhang Zhao, Hee-Joon Kim, Soo-Young Kim, Jinho Oh
  • Publication number: 20030168630
    Abstract: The invention relates to a novel synthetic route for a group of ligands and to an improved catalyst containing the ligand. It provides a method for the synthesis of a ligand having the structure: (I) The invention also provides use of a ligand for inhibiting dye transfer.
    Type: Application
    Filed: February 19, 2003
    Publication date: September 11, 2003
    Inventors: Riccardo Filippo Carina, Carl Gibson
  • Patent number: 6605599
    Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
    Type: Grant
    Filed: May 26, 1998
    Date of Patent: August 12, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson
  • Patent number: 6534649
    Abstract: Compound of formula (I): in which W1, W2 and W3, which are identical or different, each represent, independently of one another, a divalent radical chosen from those represented by the general formula (A): —[(CT5T6)a—(CT1T2)n—[N(R4)]p—(CT3T4)m—(CT7T8)b]1—  (A) as defined in the description and in which R4 represents a hydrogen atom, an alkyl radical, a [(hetero)aryl]alkyl radical or a radical represented by the general formula (B), R5—Si(X1) (X2) (X3), as defined in the description, and R1, R2 and R3, which are identical or different, each represent, independently of one another and of R4, a hydrogen atom, an alkyl radical, a [(hetero)aryl]alkyl radical comprising from 7 to 12 carbon atoms or a radical represented by the general formula (B), it being understood that the compound of formula (I) comprises more than six cyclic nitrogen atoms.
    Type: Grant
    Filed: July 24, 2000
    Date of Patent: March 18, 2003
    Assignee: L'Air Liquide, Societe Anonyme a Directoire et Conseil de Surveillance pour l'Etude et l'Exploitation des Procedes Georges Claude
    Inventors: Franck Denat, Géraud Dubois, Raphaël Tripier, Roger Guilard, Bruno Roux-Fouillet
  • Publication number: 20020193449
    Abstract: Compounds, compositions and methods are disclosed useful for enhancing penetration of a pharmacologically active substances across skin or tissue membranes. Compounds for use in such compositions and methods are highly water-soluble N-substituted polyalkylene oxide derivatives of cyclic amides.
    Type: Application
    Filed: April 10, 2001
    Publication date: December 19, 2002
    Applicant: Allergan Sales, Inc.
    Inventor: Gary Ewing
  • Patent number: 6441020
    Abstract: Compositions of matter having protein kinase C-modulatory, anti-inflammatory and other biological activities are disclosed. The compositions are derived from indolactams which have a substituent, containing at least one carbon, at the N1 position and have ether substitution on the 14-O position.
    Type: Grant
    Filed: September 28, 1998
    Date of Patent: August 27, 2002
    Assignee: Procyon Pharmaceuticals, Inc.
    Inventors: James Quick, Paul E. Driedger
  • Publication number: 20020022605
    Abstract: This invention provides compounds of Formula I having the structure 1
    Type: Application
    Filed: July 12, 2001
    Publication date: February 21, 2002
    Applicant: American Home Products Corporation
    Inventors: Fuk-Wah Sum, Baihua Hu
  • Publication number: 20020013459
    Abstract: The present invention relates to processes for the preparation of macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.
    Type: Application
    Filed: July 31, 2001
    Publication date: January 31, 2002
    Inventors: Roberta L. Dorow, Silvio Campagna, Pasquale N. Confalone, Fuqiang Jin, Zhe Wang
  • Publication number: 20010019709
    Abstract: The invention relates to compounds useful as radiosensitizers in tumor therapy.
    Type: Application
    Filed: May 7, 1999
    Publication date: September 6, 2001
    Inventors: WERNER KRAUSE, RUEDIGER LAWACZECK
  • Patent number: 6180113
    Abstract: Pharmaceutical agents that contain perfluoroalkyl-containing metal complexes are useful in tumor therapy and interventional radiology.
    Type: Grant
    Filed: February 19, 1997
    Date of Patent: January 30, 2001
    Assignee: Schering AG
    Inventors: Johannes Platzek, Ulrich Niedballa, Bernd Rad{umlaut over (u)}chel, Wolfgang Schlecker, Hanns-Joachim Weinmann, Thomas Frenzel
  • Patent number: 6127536
    Abstract: An improved synthesis for preparing a tetraamido-macrocyclic ligand, such as 5,6-Benzo-3,8,11,13-tetraoxo-2,2,9,9-tetramethyl-12,12-diethyl-1,4,7,10 -tetraazacyclotridecane, H.sub.4, in greatly improved yield and in a commercially viable manner, comprising the steps of dissolving a quantity of a 1,2-bis(2-aminoalkanamido)benzene in a solution comprised of ethyl acetate and methylene chloride to yield a first reaction solution; dissolving a quantity of a malonyl dihalide in an ethyl acetate solution to yield a second reaction solution; adding the first reaction solution and the second reaction solution to a reaction vessel containing a third reaction solution comprised of refluxing ethyl acetate solution and an acid scavenger to form a reaction mixture; and isolating a solid product comprised of the tetraamido-macrocycle directly from the reaction mixture by filtration.
    Type: Grant
    Filed: May 25, 1999
    Date of Patent: October 3, 2000
    Assignee: The Clorox Company
    Inventors: James E. Deline, Michael M. Ott, Kevin A. Klotter
  • Patent number: 6100394
    Abstract: A robust chelate complex is provided having the formula: ##STR1## wherein: M is a metal, preferably a transition metal; Z is an anionic donor atom, three of which are nitrogen, and the other is oxygen; L.sub.1 is a labile ligand;Ch.sub.1, Ch.sub.2 and Ch.sub.3 are oxidation resistant chelate groups which are the same or different and which form 5 or 6 membered rings with the metal, and Ch.sub.4 is a chelate group having the structure ##STR2## wherein R.sub.1 and R.sub.2 are the same or different and are preferably selected from the group consisting of hydrogen, halogen, methyl, and CF.sub.3 or when linked, a five or six membered ring cyclo substituent. The complex provides a stable, long-lived oxidation catalyst or catalyst activator.
    Type: Grant
    Filed: May 12, 1998
    Date of Patent: August 8, 2000
    Assignee: Carnegie Mellon University
    Inventors: Terrence J. Collins, Scott W. Gordon-Wylie
  • Patent number: 5981783
    Abstract: A chiral ligand system for transition or main group metal catalysts is disclosed. These ligands can be readily synthesized using inexpensive amino acids and diamines as starting materials. Several different transition or main group metals have been inserted into the ligands. The ligands have been shown to have a tetradhedral distortion that may contribute to enhanced chiral transfer from the catalyst to the substrate in chemical modifications of olefins and other reactive substrates. These catalysts have been demonstrated to be effective in catalyzing epoxidation of a variety of substrates.
    Type: Grant
    Filed: April 10, 1998
    Date of Patent: November 9, 1999
    Assignee: Polt Hill Institute
    Inventor: Robin L. Polt
  • Patent number: 5962498
    Abstract: Compounds having anti-inflammatory, anti-viral, protein kinase C-modulatory and other activities are disclosed. The compounds are derived from aromatic heterocyclic compounds of the indole, indene, benzofuran and benzothiophene class, each bearing an additional 6-atom chain connecting positions 3 and 4 to form a fused 9-membered ring. This invention is exemplified by 9-deshydroxymethyl-9-carboxyindolactam V.
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: October 5, 1999
    Assignee: Procyon Pharmaceuticals, Inc.
    Inventors: Paul E. Driedger, James Quick
  • Patent number: 5912238
    Abstract: The invention concerns the compounds of formula I ##STR1## wherein the substituents have various significances. They are prepared by several processes including epimerizing replacement, treatment with cyanogen bromide or thiophosgene, treatment with an acid having a non-nucleophilic anion, treatment with dimethylsulfoxide and acetic anhydride, acylation, treatment with an oxalyl derivative and ammonia, methylation, oxidation, deprotection and protection. They possess interesting pharmacological activity as antiinflammatory, immunosuppressant, antiproliferative and chemotherapeutic drug resistance reversing agents.
    Type: Grant
    Filed: July 18, 1994
    Date of Patent: June 15, 1999
    Assignee: Novartis AG
    Inventors: Karl Baumann, Gerhard Emmer
  • Patent number: 5891870
    Abstract: Compositions with anti-inflammatory and other activitites are disclosed. The compositions are derived from phorboids of the diterpene- and benzolactam-classes.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 6, 1999
    Assignee: Procyon Pharmaceuticals, Inc.
    Inventors: Paul E. Driedger, James Quick
  • Patent number: 5817292
    Abstract: This invention provides compositions useful in MR imaging comprising a polymer comprising units comprising the residue of a chelating agent linked to a poly(alkylene oxide) moiety, the polymer having a paramagetic metal ion associated therewith.
    Type: Grant
    Filed: October 14, 1992
    Date of Patent: October 6, 1998
    Assignee: Nycomed Imaging AS
    Inventors: Robert A. Snow, David L. Ladd, John L. Toner
  • Patent number: 5756688
    Abstract: This invention provides compositions useful in MR imaging comprising a polymer comprising units comprising the residue of a chelating agent linked to a poly(alkylene oxide) moiety, the polymer having a paramagetic metal ion associated therewith.
    Type: Grant
    Filed: September 14, 1993
    Date of Patent: May 26, 1998
    Assignee: Sterling Winthrop Inc.
    Inventors: Robert A. Snow, David L. Ladd, John L. Toner, K. Robert Hollister
  • Patent number: 5728710
    Abstract: Rapamycin derivatives; pharmaceutical compositions comprising such rapamycin derivatives and pharmaceutically acceptable carriers or diluents; and methods of using such derivatives to inhibit pathogenic fungi growth inhibition, inhibit immunosuppression or treat carcinogenic tumors are disclosed.
    Type: Grant
    Filed: March 16, 1995
    Date of Patent: March 17, 1998
    Assignee: SmithKline Beecham Corporation
    Inventor: Juan Ignacio Luengo
  • Patent number: 5721361
    Abstract: A process for preparing a substituted polyazamacrocycle is provided which comprises contacting a diamine or triamine and a dicarboxylic acid or ester or anhydride thereof in the presence of a suitable base and a suitable solvent to produce the substituted polyazamacrocycle provided that when an ester of said dicarboxylic acid is used, said suitable base is optional, and when said dicarboxylic acid or an anhydride of said dicarboxylic acid is used, the reaction mixture further comprises a suitable coupling agent.
    Type: Grant
    Filed: June 11, 1996
    Date of Patent: February 24, 1998
    Assignee: The Monsanto Company
    Inventors: Patrick J. Lennon, Susan L. Henke, Karl W. Aston
  • Patent number: 5690909
    Abstract: The invention relates to new fluorine-containing macrocyclic metal complexes that consist of a complexing agent of formula I and at least one metal ion of an element of atomic numbers 21-29, 42, 44 or 57-83 ##STR1## in which n, R.sup.1, R.sup.2, R.sup.3 and A have a different meaning, agents containing these compounds, their use as NMR and x-ray diagnostic agents as well as process for the production of these compounds and agents.
    Type: Grant
    Filed: March 19, 1996
    Date of Patent: November 25, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Johannes Platzek, Bernd Raduchel, Ulrich Niedballa, Hanns-Joachim Weinmann, Hans Bauer, Klaus Roth
  • Patent number: 5672605
    Abstract: Novel macrolide compounds of the formula ##STR1## and pharmaceutically acceptable salts, esters, amides and prodrugs thereof, processes for the preparation of the compounds of the invention, intermediates useful in these processes, a pharmaceutical composition, and a method of treating immunomodulatory disorders are disclosed.
    Type: Grant
    Filed: April 19, 1995
    Date of Patent: September 30, 1997
    Assignee: Abbott Laboratories
    Inventors: Yat Sun Or, Jay R. Luly, Rolf Wagner
  • Patent number: 5622821
    Abstract: The invention provides lanthanide chelates capable of intense luminescence. The celates comprise a lanthanide chelator covalently joined to a coumarin-like or quinolone-like sensitizer. Exemplary sensitzers include 2- or 4-quinolones, 2- or 4-coumarins, or derivatives thereof e.g. carbostyril 124 (7-amino-4-methyl-2-quinolone), coumarin 120 (7-amino-4-methyl-2-coumarin), coumarin 124 (7-amino-4-(trifluoromethyl)-2-coumarin), aminomethyltrimethylpsoralen, etc.The chelates form high affinity complexes with lanthanides, such as terbium or europium, through chelator groups, such as DTPA. The chelates may be coupled to a wide variety of compounds to create specific labels, probes, diagnostic and/or therapeutic reagents, etc. The chelates find particular use in resonance energy transfer between chelate-lanthanide complexes and another luminescent agent, often a fluorescent non-metal based resonance energy acceptor.
    Type: Grant
    Filed: June 29, 1994
    Date of Patent: April 22, 1997
    Assignee: The Regents of the University of California
    Inventors: Paul R. Selvin, John Hearst
  • Patent number: 5614649
    Abstract: Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: March 25, 1997
    Assignee: Cephalon, Inc.
    Inventors: Mohamed Iqbal, James L. Diebold, Robert Siman, Sankar Chatterjee, James C. Kauer
  • Patent number: 5589473
    Abstract: The present invention relates to a compound of the formula ##STR1## wherein X.sup.1, R.sup.1, R.sup.2, OP, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.0 are as described herein, and their pharmaceutically acceptable salts thereof carrying an acidic and/or basic substituent.The compound of formula I as well as their pharmaceutically acceptable salts inhibit DNA gyrase activity in bacteria and possess antibiotic, especially antibacterial activity against microorganisms and can be used in the control or prevention of infectious diseases.
    Type: Grant
    Filed: March 20, 1995
    Date of Patent: December 31, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: J urgen Geiwiz, Erwin G otschi, Paul Hebeisen, Helmut Link, Thomas L ubbers
  • Patent number: 5583219
    Abstract: A novel bifunctional macrocyclic chelating agent useful for attaching metal ions to proteins, polypeptides and other polymers. These reagents are unique in their ability to bind a variety of metal ions and to yield a high metal ion concentration per protein molecule. Protein metal chelates thus obtained will have useful radiophysical, chemical, fluorescent, photochemical and magnetic properties suitable for biomedical applications.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: December 10, 1996
    Assignee: Akzo Nobel N.V.
    Inventors: Ramaswamy Subramanian, James L. Colony
  • Patent number: 5583139
    Abstract: Novel macrolide compounds of the formula ##STR1## and pharmaceutically acceptable salts, esters, amides and prodrugs thereof, processes for the preparation of the compounds of the invention, intermediates useful in these processes, a pharmaceutical composition, and a method of treating immunomodulatory disorders are disclosed.
    Type: Grant
    Filed: April 19, 1995
    Date of Patent: December 10, 1996
    Assignee: Abbott Laboratories
    Inventors: Yat Sun Or, Jay R. Luly, Rolf Wagner
  • Patent number: 5565561
    Abstract: The invention relates to the natural substance cyclamenol of the formula ##STR1## a process for its preparation from microorganisms of the order of the Actinomycetales, in particular from the Streptomyces strain MHW 846, chemical derivatives thereof, and its use as a medicament, in particular for acute and chronic inflammatory disorders in human and veterinary medicine.
    Type: Grant
    Filed: April 27, 1995
    Date of Patent: October 15, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hartwig M uller, Erwin Bischoff, Volker-Bernd Fiedler, Karlheinz Weber, Burkhard Fugmann, Bruno Rosen
  • Patent number: 5563127
    Abstract: Novel boronic acid and ester and carboxyl-modified amino acid compounds of the Formula I, which are inhibitors of trypsin-like enzymes, are disclosed :R.sup.1 --Z--CHR.sup.2 --A,where R.sup.1, Z, R.sup.2 and A are defined within.
    Type: Grant
    Filed: December 27, 1994
    Date of Patent: October 8, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Eugene C. Amparo, William H. Miller, Gregory J. Pacofsky, John Wityak, Patricia C. Weber, John J. V. Duncia, Joseph B. Santella, III
  • Patent number: RE41893
    Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: October 26, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson
  • Patent number: RE41895
    Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: October 26, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson
  • Patent number: RE41911
    Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: November 2, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri
  • Patent number: RE43003
    Abstract: The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: December 6, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Soong-Hoon Kim, James A. Johnson